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Compound Detail

CHEMBL5598576

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O=C(NCC(F)F)[C@H](Nc1ccc2c(c1)CNC2)c1cc(Cl)cc(C2CC2)c1

Basic Information

ChEMBL ID CHEMBL5598576
Phase Preclinical
Structure Type MOL
InChI Key ZBDKUHJVDDPOHR-HXUWFJFHSA-N
4
Targets
16
Activities
2
Assay Types
18
PK Parameters
15
Publications
0
Known Names

Molecular Properties

405.9
MW (Da)
4.36
ALogP
3
HBA
3
HBD
53.2
PSA (Ų)
0.64
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H22ClF2N3O
MW 405.88
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.95

Activity Summary

IC50 11 meas. best 7.82
EC50 5 meas. best 6.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nonstructural protein 3
CHEMBL4523954
IC50 7.82 7.5417 15.0 6
NS3
CHEMBL5705861
IC50 6.89 6.62 129.0 3
Zika virus
CHEMBL4296612
EC50 6.02 5.614 964.0 5
NS3 protease
CHEMBL5705863
IC50 4.62 4.585 23817.0 2

Pharmacokinetic Data

Parameter Value Units Species
CL 10.0 mL.min-1.g-1 Homo sapiens
CL 10.0 mL.min-1.g-1 Homo sapiens
CL 10.0 mL.min-1.g-1 Homo sapiens
CL 10.0 mL.min-1.g-1 Mus musculus
CL 10.0 mL.min-1.g-1 Homo sapiens
CL 10.0 mL.min-1.g-1 Mus musculus
Fu 0.07 - Homo sapiens
Fu 0.07 - Mus musculus
Fu 0.9 - Bos taurus
Fu 0.08 - Mus musculus
Fu 0.1 - Homo sapiens
Fu 0.9 - Bos taurus
T1/2 2.888 hr Homo sapiens
T1/2 2.888 hr Homo sapiens
T1/2 2.888 hr Homo sapiens
T1/2 2.888 hr Mus musculus
T1/2 2.888 hr Homo sapiens
T1/2 2.888 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Nonstructural protein 3 IC50 = 15.0 nM 7.82 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 17.0 nM 7.77 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 23.0 nM 7.64 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 24.0 nM 7.62 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 62.0 nM 7.21 Functional biochemical assay to identify treatments for viral infectious disease... -
Nonstructural protein 3 IC50 = 65.0 nM 7.19 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 IC50 = 129.0 nM 6.89 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 IC50 = 129.0 nM 6.89 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 IC50 = 840.0 nM 6.08 Functional biochemical assay to identify treatments for viral infectious disease... -
Zika virus EC50 = 964.0 nM 6.02 Functional immunofluorescence assay to measure dose dependent changes in antivir... -
Zika virus EC50 = 1115.0 nM 5.95 Functional CPE-based assay to measure dose dependent changes in antiviral-drug i... -
Zika virus EC50 = 2630.0 nM 5.58 Functional immunofluorescence assay to measure dose dependent changes in antivir... -
Zika virus EC50 = 3162.0 nM 5.5 Functional CPE-based assay to measure dose dependent changes in antiviral-drug i... -
Zika virus EC50 = 9577.0 nM 5.02 Functional CPE-based assay to measure dose dependent changes in antiviral-drug i... -
NS3 protease IC50 = 23817.0 nM 4.62 Functional biochemical assay to identify treatments for viral infectious disease... -
NS3 protease IC50 = 28457.0 nM 4.55 Functional biochemical assay to identify treatments for viral infectious disease... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5674856 ADMET 30
- 10.6019/CHEMBL5665440 ADMET 24
- 10.6019/CHEMBL5674852 ADMET 16
- 10.6019/CHEMBL5661943 Zika virus 14
- 10.6019/CHEMBL5661955 ADMET 14
- 10.6019/CHEMBL5661943 dengue virus type 2 8
- 10.6019/CHEMBL5604063 Genome polyprotein 6
- 10.6019/CHEMBL5604062 Nonstructural protein 3 6
- 10.6019/CHEMBL5674854 No relevant target 4
- 10.6019/CHEMBL5598561 Nonstructural protein 3 3
- 10.6019/CHEMBL5604061 NS3 3
- 10.6019/CHEMBL5604064 NS3 protease 3
- 10.6019/CHEMBL5604065 NS3 protease 3
- 10.6019/CHEMBL5604066 NS3 protease 3
- 10.6019/CHEMBL5674850 No relevant target 3

Data from ChEMBL 36 via Core Engine